Antihistamines block the effects of histamine in the body and are used to treat allergy symptoms and other conditions. They work by antagonizing H1 and H2 receptors. First generation antihistamines have sedative effects while second generation mainly have antihistaminic effects. Common brands include Benadryl, Claritin, Zyrtec and Pepcid with recommended dosages provided.
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Antihistamines Pharmacology
Antihistamines block the effects of histamine in the body and are used to treat allergy symptoms and other conditions. They work by antagonizing H1 and H2 receptors. First generation antihistamines have sedative effects while second generation mainly have antihistaminic effects. Common brands include Benadryl, Claritin, Zyrtec and Pepcid with recommended dosages provided.
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ANTIHISTAMINES
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WHAT IS ANTIHISTAMINES?
An antihistamine is a prescription or over-the-
counter medication that blocks some of what histamine does. HOW DOES ANTIHISTAMINES WORK?
An Antihistamines block the effects of a substance
called histamine in your body. Histamine is normally released when your body detects something harmful, such as an infection. It causes blood vessels to expand and the skin to swell, which helps protect the body. MECHANISM OF ACTION Histamine (an endogenous chemical messenger) induces an increased level of vascular permeability, which leads to fluid moving from capillaries into the surrounding tissues. The overall outcome of this is increased swelling and dilation of vessels. Antihistamines stop this effect by acting as antagonists at the H-1 receptors. The clinical benefit is a reduction in allergy symptoms and any related symptoms. CLASSIFICATION OF ANTIHISTAMINES
H-1 receptor antagonists or H-1 blockers. This subtype of
antihistamines is used to treat allergy symptoms. The H-1 blocker subtype is further broken down into two groups — first- generation antihistamines and second-generation antihistamines.
H-2 receptor antagonists or H-2 blockers. They are used to treat
gastrointestinal conditions, including gastroesophageal reflux disease [GERD] (also called acid reflux), peptic ulcers, gastritis, motion sickness, nausea and vomiting. DIFFERENCE BETWEEN FIRST AND SECOND GENERATION ANTIHISTAMINES
FIRST-GENERATION ANTIHISTAMINES- beside their antihistaminic
effect (neutralizing allergy, itching, edema), they have sedative effect for (for pain and sleep), antiemetic effect (for nausea and vomiting), and anticholinergic effect (for runny nose).
SECOND-GENERATION ANTIHISTAMINES- have mainly
antihistaminic effect, ,with no or very little sedation, anticholinergic, antiemetic effects ANTIHISTAMINES BRAND EXAMPLES AND RECOMMENDED DOSAGE Examples of first-generation over-the-counter and prescription H-1 blockers BRAND NAMES RECOMMENDED DOSAGE
Brompheniramine (Children’s 10mL every 4 hours; max 6 doses/24 hours
Dimetapp Cold®) Chlorpheniramine (Chlor-Trimeton®) One tablet every 4-6 hours, not to exceed 6 tablets in 24 hours Clemastine (Dayhist®) 1.34 mg PO q12hr; not to exceed 8.04 mg/day for syrup or 2.68 mg/24 hours for tablets Cyproheptadine (Periactin®) 4 mg PO q8hr initially